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WO2012035468A2 - Composition topique moussante - Google Patents

Composition topique moussante Download PDF

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Publication number
WO2012035468A2
WO2012035468A2 PCT/IB2011/053922 IB2011053922W WO2012035468A2 WO 2012035468 A2 WO2012035468 A2 WO 2012035468A2 IB 2011053922 W IB2011053922 W IB 2011053922W WO 2012035468 A2 WO2012035468 A2 WO 2012035468A2
Authority
WO
WIPO (PCT)
Prior art keywords
foamable composition
composition
concentration
present
oil
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/IB2011/053922
Other languages
English (en)
Other versions
WO2012035468A3 (fr
Inventor
David Marcos
Milane Haran
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
TRIMA - ISRAEL PHARMACEUTICAL PRODUCTS MAABAROT Ltd
Original Assignee
TRIMA - ISRAEL PHARMACEUTICAL PRODUCTS MAABAROT Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by TRIMA - ISRAEL PHARMACEUTICAL PRODUCTS MAABAROT Ltd filed Critical TRIMA - ISRAEL PHARMACEUTICAL PRODUCTS MAABAROT Ltd
Priority to EP11776533.9A priority Critical patent/EP2616037A2/fr
Publication of WO2012035468A2 publication Critical patent/WO2012035468A2/fr
Priority to IL225193A priority patent/IL225193A0/en
Anticipated expiration legal-status Critical
Publication of WO2012035468A3 publication Critical patent/WO2012035468A3/fr
Ceased legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04—Dispersions; Emulsions
    • A61K8/046—Aerosols; Foams
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/28—Compounds containing heavy metals
    • A61K31/315—Zinc compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
    • A61K31/728—Hyaluronic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04—Dispersions; Emulsions
    • A61K8/06—Emulsions
    • A61K8/064—Water-in-oil emulsions, e.g. Water-in-silicone emulsions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/27—Zinc; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/12—Aerosols; Foams
    • A61K9/122—Foams; Dry foams
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
    • A61K2800/30—Characterized by the absence of a particular group of ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/74—Biological properties of particular ingredients
    • A61K2800/75—Anti-irritant

Definitions

  • the present invention relates to the field of chemical compositions, and more specifically to a foamable composition for topical application, the composition comprising a water in oil emulsion.
  • Topical application involves the absorption of a formulation by and/or through skin, mucous membrane or wound tissue. Topical applications may also be used to protect the skin or mucous membrane from external irritants such as chemicals, biological fluids, sunlight, etc.
  • ointments containing white petroleum as the carrier often form an impermeable barrier, so that metabolic products and excreta from the area to which they are applied are not easily removed or drained away. Furthermore, it may be difficult for an active agent dissolved in the carrier to pass through the white petrolatum barrier layer to the skin, so the efficacy of the drug is reduced. In addition, ointments and creams often do not create an environment for promoting normal respiration of the skin.
  • Foams for topical application are pressurized delivery forms containing one or more ingredients that, upon valve actuation, emit a fine dispersion of liquid and/or solid materials in a gaseous medium.
  • Topical foams utilize compressed gases of various types as propellants, including but not limited to hydrocarbon gases (propane, butane, and isobutane), nitrogen, carbon dioxide, freons, chlorofluorocarbons, and fluorocarbons.
  • Foam formulations are generally easier to apply, are less dense, and spread more easily than other topical dosage forms. Foams may be formulated in various ways to provide emollient or drying functions to the skin, depending on the formulation constituents.
  • Emulsion systems provide a two-phase system including lipophilic or hydrophobic components in one phase and hydrophilic components in the second phase.
  • the foamed emulsion typically is an oil-in-water emulsion in which the hydrophobic component is dispersed in the aqueous continuous phase.
  • WO 04/037225 discloses an oil in water emulsion comprising 80-98% water
  • US 20040106688 discloses an oil in water emulsion comprising from 50 to 97% by weight of a water phase.
  • US 20080044444 discloses foamable compositions comprising a dicarboxylic acid or ester derivative thereof in which the dicarboxylic acid or ester derivative is a stabilizing emollient and or has a therapeutic effect.
  • US 20060281823 discloses a foamable water-in-oil type emulsion composition comprising diglyceride-containing fats and oils and a liquid sugar, having improved in-mouth meltability and thermostability with a low specific gravity and a good eating texture for use in buttercreams or similar products.
  • the application does not disclose the use of such a composition comprising an active pharmaceutical ingredient.
  • Foams and, in particular, foam emulsions are complicated systems which do not form under all circumstances. Slight shifts in foam emulsion composition, such as by the addition of active ingredients, may destabilize the foam.
  • WO 2007/007208 discloses a water in oil foam composition comprising a plurality of surfactants, wherein a total Hydrophilic-lipophilic balance ("HLB") for a water in oil composition is stated as being between about 2 and about 9.
  • the formulations in this application include at least one gelling agent, which control the residence of the composition in the target site. Self-spreading of the foam is thus limited in the prior art composition. Addition of gelling agents often complicates manufacture of the product as these agents are sometimes difficult to dissolve, they may form lumps and usually greatly increase production times and costs.
  • the prior art does not disclose a foamable, water in oil emulsion for topical application, which is devoid of a gelling agent and/or benzalkonium chloride.
  • the present invention provides a foamable composition for topical application, the composition comprising a water in oil emulsion, which is devoid of a gelling agent and/or benzalkonium chloride.
  • the present invention provides, in at least some embodiments, a foamable composition comprising an emulsion for topical application.
  • the composition may comprise a water in oil emulsion. According to other embodiments of the present invention, the composition may comprise an oil in water emulsion.
  • composition of the present invention may be particularly useful for treatment and/or prevention of one or more skin conditions, for example, as described in detail below..
  • the composition may include one or more components and/or properties to enable the treatment and/or prevention of one or more skin conditions, e.g., as described herein.
  • the composition described herein may be effective for the treatment and/or prevention of one or more skin conditions, e.g., as described herein, while being devoid of one or more components, for example, one or more components that may cause irritation to the skin, for example, while being devoid of a gelling agent and/or a preservative, e.g., benzalkonium chloride.
  • a gelling agent and/or a preservative e.g., benzalkonium chloride.
  • the present invention provides a foamable composition
  • a foamable composition comprising a water in oil emulsion, the emulsion comprising, for example, up to about 40% (w/w) oil and up to about 60% (w/w) water.
  • the present invention provides a foamable composition
  • a foamable composition comprising a water in oil emulsion, the emulsion comprising up to about 40% (w/w) oil, up to about 60% (w/w) water and at least one surfactant., providing, for example, a total HLB of less than about 7.
  • the composition may comprise an emulsion, the emulsion comprising at least one of zinc oxide, hyaluronic acid or zinc hyaluronate, optionally as an active ingredient, although the use of other active ingredients, including natural ingredients of plant and/or animal origin, such as, for example, Euphrasia Mallow, Chamomile, Hamamelis, or Aloe is considered as being within the scope of the invention.
  • active ingredients including natural ingredients of plant and/or animal origin, such as, for example, Euphrasia Mallow, Chamomile, Hamamelis, or Aloe is considered as being within the scope of the invention.
  • Zinc oxide is commonly used to treat minor burns and skin irritation, and is a preferred ingredient in many creams and ointments for the treatment or prevention of various skin conditions, e.g., diaper rash.
  • the foamable composition may comprise a water in oil emulsion comprising at least one surfactant, providing a total HLB of less than about 7, wherein the composition is devoid of a gelling agent.
  • the emulsion may further comprise at least one of zinc oxide, hyaluronic acid, zinc hyaluronate or a plant extract.
  • the composition may comprise up to about 25% (w/w of total composition) zinc oxide.
  • zinc oxide is preferably present at a concentration in the range of from about 2% to about 20% w/w of total composition, more preferably about 10% w/w of total composition.
  • the composition may further comprise up to about 40% (w/w of total composition) oil as a carrier in a water in oil emulsion.
  • the oil described herein may have a certain degree of polarity.
  • polarity is a measure of the unequal distribution of electrons across a molecule. Different level of polarity may be attributed to different molecules according to their atom content and/or structure.
  • Polar oils may contain heteroatoms that differ in electronegativity. This results in a dipole moment.
  • Typical polar oils are fatty alcohols, esters and triglycerides.
  • An example of a polar molecule is water, wherein the electrons are not evenly distributed thus creating a dipole.
  • Nonpolar oils may be hydrocarbons. They lack an electronegative element like oxygen, which results in their typical hydrocarbon feel.
  • An example of a non-polar molecule is the methane molecule. In the methane molecule (CH 4 ) the four C-H bonds are arranged tetrahedrally around the carbon atom. Each bond has a certain polarity (though not very strong in this case). However, the bonds are arranged symmetrically so there is no overall dipole in the molecule.
  • the degree of polarization of a bond may be measured in percent ionic character, and one can determine this value from the difference in electronegativity of two atoms using various methods (El-Mahrab-Robert et al, Assessment of oil polarity: Comparison of evaluation methods, International Journal of Pharmaceutics 348 (2008) 89-94).
  • water contains the bond O-H between oxygen and hydrogen.
  • the electronegativity of O is 3.5 and H is 2.1, so they differ by 1.4.
  • On a chart of ionic character one may find this bond is 39 percent ionic, thus a compound containing O-H will be quite polar.
  • the ionic character of a carbon-hydrogen bond is only 4 percent, so a compound containing only C-H would be nonpolar.
  • some oils described herein may contain few charged molecules, and may be referred to herein as having low polarity. According to other embodiments, some oils described herein may contain charged molecules and may be referred to herein as having medium and/or high polarity.
  • the oil of the present invention may have a low polarity and may include, for example, one or more of mineral oil, triglyceride oil, squalane, tocopherol or its derivatives, avocado oil, macadamia oil, corn oil, olive oil, sesame oil, peanut oil, octyl dodecanate, or oleic acid decyl ester, or combinatations thereof.
  • the oil may have a medium to high polarity.
  • suitable oils may include isopropyl myristate, isopropyl palmitate, caprylic / capric triglycerides, propylene glycol dicaprylate / dicaprate, decyl oleate, dibutyl adipate, or hexyl laurate, or combinations thereof.
  • the oil may include a combination of a low polarity oil and a medium to high polarity oil.
  • the oil of the present invention comprises isopropyl myristate and mineral oil.
  • the mineral oil is optionally and preferably present at a concentration of from about 20 to about 40% w/w of total composition, and said isopropyl myristate is present at a concentration of from about 5 to about 15% and more preferably from about 6 to about 10%, w/w of total composition.
  • the composition may comprise at least one surfactant, the surfactant or combination of surfactants may provide a total HLB of less than about 7.
  • at least one surfactant may comprise a fatty acid ester having an HLB of less than about 7.
  • Suitable fatty acid esters may include but are not limited to sorbitan fatty acid esters (such as sorbitan monolaurate; sorbitan mono palmitate; sorbitan monooleate, sorbitan dioleate; sorbitan trioleale; sorbitan sesquioleate; sorbitan monolaurate; sorbitan monoisostearate; sorbitan diisostearate; sorbitan sesquistearate); sucrose fatty acid esters (such as sucrose monopalmitate; sucrose monostearate; sucrose distearate; sucrose polystearate); propylene glycol fatty acid esters (such as propylene glycol stearate; propylene glycol alginate); glyceryl fatty acid esters (such as glyceryl monooleate; glyceryl monostearate; glyceryl myristate).
  • sorbitan fatty acid esters such as sorbitan monolaurate;
  • the fatty acid ester surfactant may comprise glyceryl monooleate. More preferably, the glyceryl monooleate is present at a concentration in the range of from about 0.1% to about 7% w/w of total composition, and most preferably, in the range of from about 0.1 to about 3.5% w/w of total composition.
  • the fatty acid ester surfactant may comprise sucrose polystearate.
  • sucrose polystearate is present at a concentration of up to about 6% w/w of total composition.
  • sucrose polystearate is present at a concentration of from about 0.3% to about 2% w/w of total composition.
  • the fatty acid ester surfactant may comprise sucrose polystearate and sucrose distearate.
  • sucrose polystearate is present at a concentration of up to about 3% w/w of total composition
  • sucrose distearate is present at a concentration of up to about 1% w/w of total composition.
  • sucrose polystearate is present at a concentration of about 0.3% w/w of total composition
  • sucrose distearate is present at a concentration of about 0.1% w/w of total composition.
  • the fatty acid surfactant may comprise sucrose distearate.
  • sucrose distearate is present at a concentration of up to about 4% w/w of total composition.
  • sucrose distearate is present at a concentration of from about 0.3% to about 1 % w/w of total composition.
  • the composition may further comprise a co-emulsifier, such as, for example, beeswax, lanolin, cetyl alcohol, stearyl alcohol, cetostearyl alcohol, stearic acid, or palmitic acid.
  • a co-emulsifier such as, for example, beeswax, lanolin, cetyl alcohol, stearyl alcohol, cetostearyl alcohol, stearic acid, or palmitic acid.
  • the beeswax may be present at a concentration of up to about 6% w/w of total composition.
  • the beeswax is present at a composition of from about 2% to about 5% w/w of total composition.
  • lanolin is present at a concentration of up to about 7% w/w of total composition.
  • the lanolin is present at a concentration of from about 2% to about 5% w/w of total composition.
  • the composition of the present invention may further comprise panthenol.
  • Panthenol may act as a humectant, emollient and/or moisturizer, for example, to improve hydration, reduce itching and/or inflammation of the skin, accelerate and/or improve healing of wounds, e.g., epidermal wounds.
  • panthenol is present at a concentration of up to about 5% w/w of total composition.
  • panthenol is present at a concentration of about 2% w/w of total composition.
  • the composition of the present invention may further comprise aloe vera extract, for example, in an amount effective in the treatment of wounds and/or skin irritations.
  • the aloe vera extract is present at a concentration of up to about 1% w/w of total composition.
  • the aloe vera extract is present at a concentration of about 0.1% w/w of total composition.
  • the composition of the present invention may further comprise a preservative (such as, for example, benzalkonium chloride, sodium benzoate, benzoic acid, benzyl alcohol, a paraben or salt thereof, imidurea, potassium sorbate, sorbic acid, phenoxyethanol, chlorocresol, or bronopol, or mixtures thereof).
  • a preservative such as, for example, benzalkonium chloride, sodium benzoate, benzoic acid, benzyl alcohol, a paraben or salt thereof, imidurea, potassium sorbate, sorbic acid, phenoxyethanol, chlorocresol, or bronopol, or mixtures thereof.
  • a paraben may be used, for example, to act as a preservative.
  • the paraben may be selected from the group consisting of methyl paraben, methyl paraben sodium, propyl paraben, propyl paraben sodium, or mixtures thereof.
  • At least one of methyl paraben and methyl paraben sodium is present at a concentration of up to about 0.2%, and more preferably at a concentration of about 0.18% w/w of total composition.
  • propyl paraben and propyl paraben sodium is present at a concentration of up to about 0.1%, and more preferably at a concentration of about 0.02 % w/w of total composition.
  • a preservative such as benzalkonium chloride may be present in the composition, e.g., at a concentration of up to about 1% w/w of total composition. In some embodiments, the preservative may be present at a concentration of about 0.2% w/w of total composition.
  • Benzalkonium chloride also known as alkyldimethylbenzylammonium chloride (ADBAC) is a mixture of alkylbenzyldimethylammonium chlorides of various even-numbered ⁇ alkyl chain lengths. This product is a nitrogenous cationic surface-acting agent belonging to the quaternary ammonium group.
  • ADBAC alkyldimethylbenzylammonium chloride
  • Standard concentrates are manufactured as 50% and 80% w/w solutions, and sold under trade names such as BC50, BC80, BAC50, BAC80, etc.
  • Benzalkonium chloride solutions of 10% or more are toxic to humans, causing irritation to the skin and mucosa.
  • concentrations of less than 10% when used as preservative in foam compositions, may have irritant effects on human skin, particularly in combination with certain other excipients.
  • the composition may comprise at least one surfactant and may be devoid of benzalkonium chloride.
  • the present invention may provide a foamable composition comprising an emulsion, said emulsion comprising at least one surfactant and being devoid of of benzalkonium chloride, for use in treating a skin condition.
  • the composition of the present invention may further comprise a surfactant selected from the group consisting of self emulsifying surfactants such as glyceryl stearate (with) PEG- 100 stearate (e.g. Arlacel 170®, Simulsol 165®, ), sorbitan stearate (with) sucrose cocoate (e.g. Arlatone 2121®), PEG-30 dipolyhydroxystearate (e.g. Arlacel)
  • self emulsifying surfactants such as glyceryl stearate (with) PEG- 100 stearate (e.g. Arlacel 170®, Simulsol 165®, ), sorbitan stearate (with) sucrose cocoate (e.g. Arlatone 2121®), PEG-30 dipolyhydroxystearate (e.g. Arlacel)
  • ceteth-2 e.g. Brij 52®
  • 100 stearate and sorbitant stearate (with) sucrose cocoate may be present at a concentration of up to about 1%, and more preferably about 0.2% w/w of total composition.
  • PEG-30 dipolyhydroxystearate may be present at a concentration of up to about 1%, and more preferably about 0.4% w/w of total composition.
  • ceteth-2 may be present at a concentration of up to about 5%, and more preferably about 3% w/w of total composition.
  • the composition of the present invention may further comprise Bisabolol, preferably at a concentration of up to about 1% w/w of the total composition and more preferably, at a concentration of about 0.2% w/w of the total composition.
  • Bisabolol a derivative of M. chamomilla (German chamomile)
  • M. chamomilla German chamomile
  • the composition of the present invention may further comprise at least one of a chelating agent, such as EDTA as well as its sodium or calcium salts; a solvent, for example a hydrophilic liquid, such as propylene glycol or glycerin; an emulsion stabilizer, such as magnesium sulfate, or combinations thereof.
  • a chelating agent such as EDTA as well as its sodium or calcium salts
  • a solvent for example a hydrophilic liquid, such as propylene glycol or glycerin
  • an emulsion stabilizer such as magnesium sulfate, or combinations thereof.
  • the chelating agent may comprise disodium EDTA, more preferably at a concentration of up to about 1% w/w of total compsosition, most preferably at a concentration of about 0.3% w/w of total composition.
  • the hydrophilic liquid may comprise propylene glycol, more preferably at a concentration of from about 1 % to about 3% w/w of total composition, most preferably at a concentration of about 2% w/w of total compositon.
  • the emulsion stabilizer may comprise magnesium sulfate, more preferably at a concentration of up to about 1% w/w of total composition, most preferably at a concentration of about 0.2% w/w of total compositon.
  • the emulsion stabilizer may comprise xanthan gum, more preferably at a concentration of up to about 1% w/w of total composition, most preferably at a concentration of about 0.25% w/w of total compositon.
  • the foamable composition of the present invention may be adapted for delivery from a pressurized container, for example, wherein a foam may be formed upon expulsion from the container.
  • the composition may further comprise at least one propellant, such as, for example, one or more hydrocarbon gases (propane, butane and isobutane) and/or fluorocarbons (such as Dymel 134a®).
  • propellant such as, for example, one or more hydrocarbon gases (propane, butane and isobutane) and/or fluorocarbons (such as Dymel 134a®).
  • composition of the present invention may be useful, in some embodiments, for the treatment and/or prevention of a skin condition, such as, for example, diaper rash, psoriasis, eczema, urticaria, scabies, acne, alopecia areata, bullous pemphigoid, dermatitis (including contact dermatitis, atopic dermatitis, dermatitis herpetiformis, seborrheic dermatitis, nummular dermatitis, stasis dermatitis, and perioral dermatitis), eczema, urticaria, scabies, acne, alopecia areata, bullous pemphigoid, impetigo, keloids, pruritis, rosacea, vitiligo, burns, irritation, inflammation, fungal infection, dry skin, skin allergies, diabetic skin conditions, decubitus ulcers and the like.
  • a skin condition such as, for example, diaper rash
  • the composition may be useful for the treatment and/or prevention of one or more skin conditions which may occur and/or develop due to one or more of rubbing, chafing, abrasion and the like.
  • the composition may be used by people and/or patients which may be more prone to develop one or more of the above mentioned skin conditions, such as, athletes, e.g., bicycle riders and runners, soldiers, obese people, and the like.
  • a person may be considered as obese when the Body mass index (BMI) greater than 30 kg/m 2 .
  • BMI Body mass index
  • the composition of the present invention may be useful, in some embodiments, for providing a skin soothing and anti-itching effect.
  • composition of the present invention may preferably be useful for treatment and/or prevention of skin conditions such as dermatitis, including diaper dermatitis (diaper rash), both in infants and in incontinent adults.
  • treating may include abrogating, substantially inhibiting, slowing and/or reversing the progression of a condition, substantially ameliorating clinical and/or aesthetical symptoms of a condition and/or substantially preventing and/or diminishing the appearance of clinical and/or aesthetical symptoms of a condition.
  • Diaper rash is a generalized term indicating any skin irritation, regardless of cause, that develops in the diaper-covered region. While diaper rash is generally thought to affect infants and toddlers, any individual wearing a diaper (for example, an incontinent adult) is a candidate to develop this condition. Contact dermatitis is the most common category of diaper rash. Skin involvement may vary from mild redness to erosion of the top layers of skin. Other categories include skin infections and allergic reactions. It is very important that no excipient which may result in irritation of the skin be present in a composition for treatment of diaper rash, especially when the formulation s used on the highly sensitive skin of an infant or toddler.
  • the foam formulations and/or compositions of the present invention may be particularly useful for treatment and/or prevention of diaper rash in incontinent adult patients, such as geriatric patients, or physically or mentally handicapped adults.
  • a formulation for prevention of diaper rash must often be administered by a single carer, using one hand, while raising and holding the posterior region of the patient with the other hand.
  • Foam formulations may be significantly easier to apply in such circumstances than other dosage forms which must be applied and/or spread by hand.
  • application of a foam composition does not require the hand of the carer to contact the skin of the patient, hence the hand does not have to be carefully cleaned, or a sterile glove changed, immediately after use.
  • a patient suffering from soreness due to diaper rash experiences less discomfort due to contact with the hand of a carer during application of the composition.
  • use of a composition as described herein in accordance with some demonstrative embodiments may prevent or diminish embarrassment to the patient and care giver who is required to apply the product to intimate parts of the patient.
  • Oil in water foam compositions may be problematic for treatment of diaper rash, for example, since the composition may be easily washed away by the urine and/or fecal excretions of a subject.
  • Water in oil compositions are preferable in this respect; however, stable water in oil foaming compositions are more difficult to formulate.
  • the composition of the present invention may preferably be dispensed from a pressurized container in an amount which provides a suitable volume for containment within a diaper, without oozing outwards. According to some embodiments.
  • the absence of a gelling agent in the foam composition of the present invention may preferably provide a foam which is less stable than conventional foams, and which is not limited to residence at the application site, enabling, for example, self- spreading of the foam upon application from a pressurized container.
  • the composition of the present invention may be a cosmetic composition for topical application. Such a composition may be useful for improving the appearance and/or texture of the skin.
  • the composition of the present invention may be provided as a medical device.
  • compositions suitable for use in the context of the present invention include compositions wherein the active ingredient is contained in an amount effective to achieve the intended purpose. More specifically, a "therapeutically effective amount” means an amount of active ingredient effective to prevent, alleviate, or ameliorate a skin and/or mucous membrane condition.
  • Example 4 Material Amount (% w/w)
  • the reduction and/or prevention of skin conditions and/or irritations due to the use of one or more of the compositions described hereinabove is assessed in a clinical trial.
  • a first group of 50 athletes (“the first group”) applies a suitable amount of a composition described hereinabove prior to conducting physical exercise, such as riding a bicycle, for 3 hours.
  • a second group of 50 athletes (“the second group”) applies a placebo composition prior to conducting a similar physical excercise for 3 hours.
  • the efficiency is based on preventing and/or diminishing one or more of the following skin conditions: skin irritations, eczema, urticaria, burns, irritation, inflammation, fungal infection, dry skin and skin allergies.
  • the assessments for efficiancy are ascertained by comparing the post- exercise skin condition of athletes from the first group to the post- exercise skin condition of athletes from the second group. Results of the clinical study demonstrate that 12 athletes from the first group develope a skin condition in comparison to 29 athletes from the second group which develop a skin condition.
  • Example 33 Treatment and/or prevention of skin condition in obese
  • the reduction and/or prevention of skin conditions and/or irritations due to the use of one or more of the compositions described hereinabove is assessed in a clinical trial.
  • a first group of 34 obese people (“the first group”) applies a suitable amount of a composition described hereinabove onto different parts of the body prone to develop skin condition, for example, skin folds and the like, three times a day for two weeks.
  • a second group of 35 obese people (“the second group”) applies a placebo composition onto different parts of the body prone to develop skin condition, three times a day for two weeks.
  • the efficiency is based on preventing and/or diminishing one or more of the following skin conditions: skin irritations, eczema, urticaria, burns, irritation, inflammation, fungal infection, dry skin and skin allergies.
  • the assessments for efficiancy are ascertained by comparing the skin condition of obese from the first group to the skin condition of obese from the second group.
  • Results of the clinical study demonstrate that 3 obese from the first group developed a skin condition in comparison to 24 obese from the second group which developed a skin condition.

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  • Epidemiology (AREA)
  • Dermatology (AREA)
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Abstract

L'invention concerne une composition moussante pour application topique, la composition comprenant une émulsion eau dans huile qui est dépourvue d'agents gélifiants.
PCT/IB2011/053922 2010-09-14 2011-09-07 Composition topique moussante Ceased WO2012035468A2 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP11776533.9A EP2616037A2 (fr) 2010-09-14 2011-09-07 Composition topique moussante
IL225193A IL225193A0 (en) 2010-09-14 2013-03-13 Foamed compound for topical use

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US38288810P 2010-09-14 2010-09-14
US38264810P 2010-09-14 2010-09-14
US61/382,888 2010-09-14
US61/382,648 2010-09-14

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WO2012035468A2 true WO2012035468A2 (fr) 2012-03-22
WO2012035468A3 WO2012035468A3 (fr) 2014-01-23

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WO (1) WO2012035468A2 (fr)

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US9067978B2 (en) 2012-10-09 2015-06-30 Novartis Ag Solution phase processes for the manufacture of macrocyclic depsipeptides and new intermediates
US9114110B2 (en) 2011-04-20 2015-08-25 Novartis Ag Suspension type topical formulations comprising cyclic depdipeptide
US9127044B2 (en) 2007-08-17 2015-09-08 Novartis Ag Cyclic depsipeptides
US9278997B2 (en) 2011-04-20 2016-03-08 Novartis Ag Processes for the manufacture of macrocyclic depsipeptides and new intermediates
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US10226483B2 (en) 2013-08-08 2019-03-12 Novan, Inc. Topical compositions and methods of using the same
US10912743B2 (en) 2016-03-02 2021-02-09 Novan, Inc. Compositions for treating inflammation and methods of treating the same
US11077194B2 (en) 2012-03-14 2021-08-03 Novan, Inc. Nitric oxide releasing pharmaceutical compositions
US11285098B2 (en) 2013-02-28 2022-03-29 Novan, Inc. Topical compositions and methods of using the same
US11285171B2 (en) 2018-03-01 2022-03-29 Novan, Inc. Nitric oxide releasing suppositories and methods of use thereof

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CN103230620A (zh) * 2013-05-10 2013-08-07 李宏江 烧烫伤急救湿敷药巾
CN112870223A (zh) * 2021-03-22 2021-06-01 佛山市邦孚新材料科技有限公司 一种婴儿护臀组合物
EP4351509A1 (fr) * 2021-06-11 2024-04-17 Edgewell Personal Care Brands, LLC Compositions et produits de soins personnels

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US9127044B2 (en) 2007-08-17 2015-09-08 Novartis Ag Cyclic depsipeptides
US9114110B2 (en) 2011-04-20 2015-08-25 Novartis Ag Suspension type topical formulations comprising cyclic depdipeptide
US9278997B2 (en) 2011-04-20 2016-03-08 Novartis Ag Processes for the manufacture of macrocyclic depsipeptides and new intermediates
US11077194B2 (en) 2012-03-14 2021-08-03 Novan, Inc. Nitric oxide releasing pharmaceutical compositions
US8987413B2 (en) 2012-10-09 2015-03-24 Novartis Ag Aldehyde acetal based processes for the manufacture of macrocyclic depsipeptides and new intermediates
US9067978B2 (en) 2012-10-09 2015-06-30 Novartis Ag Solution phase processes for the manufacture of macrocyclic depsipeptides and new intermediates
US9493512B2 (en) 2012-10-09 2016-11-15 Novartis Ag Solution phase processes for the manufacture of macrocyclic depsipeptides and new intermediates
US11285098B2 (en) 2013-02-28 2022-03-29 Novan, Inc. Topical compositions and methods of using the same
US10828323B2 (en) 2013-08-08 2020-11-10 Novan, Inc. Topical compositions and methods of using the same
US10226483B2 (en) 2013-08-08 2019-03-12 Novan, Inc. Topical compositions and methods of using the same
US10206947B2 (en) 2013-08-08 2019-02-19 Novan, Inc. Topical compositions and methods of using the same
US11813284B2 (en) 2013-08-08 2023-11-14 Novan, Inc. Topical compositions and methods of using the same
EP3177262A4 (fr) * 2014-08-08 2018-04-18 Novan Inc. Émulsions topiques
US10912743B2 (en) 2016-03-02 2021-02-09 Novan, Inc. Compositions for treating inflammation and methods of treating the same
US11285171B2 (en) 2018-03-01 2022-03-29 Novan, Inc. Nitric oxide releasing suppositories and methods of use thereof

Also Published As

Publication number Publication date
WO2012035468A3 (fr) 2014-01-23
EP2616037A2 (fr) 2013-07-24
US20120064013A1 (en) 2012-03-15

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